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发明授权
US08163909B2 Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use 有权
取代的羟乙基胺化合物作为β-分泌酶调节剂和使用方法

Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
摘要：
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I or Formula II wherein R1a, R1b, R1c, B, R3, R4, R5 and W of Formula I, and R1a, R1b, R1c, R2, R2a, R3, R4, R5, A1, A2, A3, A4, W, X, Z, m and n of Formula II are defined herein. The invention also provides compounds of Formula III, sub-Formulas II-A-II-D, sub-Formulas III-A-III-D and Formula IV. The invention further includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, AD, cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formulas I, II, III, IV and sub-formulas thereof, intermediates and processes useful for the preparation of compounds of Formulas I, II, III, IV and sub-formulas thereof.
摘要（中）：

本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I或式II，其中式I的R 1a，R 1b，R 1c，B，R 3，R 4，R 5和W以及R 1a，R 1b，R 1c，R 2，R 2a，R 3，R 4，R 5 ，式II中的A1，A2，A3，A4，W，X，Z，m和n定义。 本发明还提供了式III化合物，分子式II-A-II-D，分子式III-A-III-D和式IV的化合物。 本发明还包括这些化合物在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这些疾病包括例如AD，认知缺陷和损伤，精神分裂症和其他类似的中枢神经系统病症。 本发明还包括式I，II，III，IV及其分式的其它实施方案，可用于制备式I，II，III，IV及其子式化合物的中间体和方法。

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